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MDL 72832: a potent and stereoselective ligand at central and peripheral 5-HT1A receptors

Mir, A. K., Hibert, M., Tricklebank, M. D., Middlemiss, D. N., Kidd, Emma Jane ORCID: and Fozard, J. R. 1988. MDL 72832: a potent and stereoselective ligand at central and peripheral 5-HT1A receptors. European Journal of Pharmacology 149 (1-2) , pp. 107-120. 10.1016/0014-2999(88)90048-9

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In receptor binding assays (±)MDL 72832, 8-[4-(1,4-benzodioxan-2-ylmethylamino)butyl]8-azaspiro[4,5]decane-7,9-dione, was a potent (pIC50 9.1), selective and stereospecific ligand for central 5-HT1A recognition sites. In functional tests, (±)MDL 72832 and its S(−) and R(+) enantiomers blocked stereoselectively the 8-OH-DPAT-induced neuronal inhibition of the transmurally stimulated guinea-pig ileum and the cardiovascular effects of 8-OH-DPAT in anaesthetized rats. In contrast, (±)MDL 72832 and its enantiomers were exclusively ‘8-OH-DPAT-like’ in their ability to fully and stereoselectively generalize to the 8-OH-DPAT discriminative stimulus and, in reserpinised rats, to induce forepaw treading and flat body posture. These results characterize (±)MDL 73832 as a potent, stereoselective ligand with mixed agonist and antagonist properties at central and peripheral 5-HT1A receptors. The similar stereoselective requirements for the recognition site and functional effects provides compelling evidence that the 5-HT1A recognition site is indeed a functional receptor.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Pharmacy
Subjects: R Medicine > RM Therapeutics. Pharmacology
Uncontrolled Keywords: MDL 72832; 5-HT1A receptors; Cardiovascular system; Interoceptive cue; Guinea-pig ileum; 8-OH-DPAT; (Stereoselectivity, Agonist, Antagonist, Behaviour, Rat)
Publisher: Elsevier
ISSN: 0014-2999
Last Modified: 18 Oct 2022 13:38

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